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European Journal of Drug Metabolism and Pharmacokinetics

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https://www.readbyqxmd.com/read/28374336/therapeutic-potential-and-utility-of-elacridar-with-respect-to-p-glycoprotein-inhibition-an-insight-from-the-published-in-vitro-preclinical-and-clinical-studies
#1
Ranjeet Prasad Dash, R Jayachandra Babu, Nuggehally R Srinivas
The occurrence of efflux mechanisms via Permeability-glycoprotein (P-gp) recognized as an important physiological process impedes drug entry or transport across membranes into tissues. In some instances, either low oral bioavailability or lack of brain penetration has been attributed to P-gp mediated efflux activity. Therefore, the objective of development of P-gp inhibitors was to facilitate the attainment of higher drug exposures in tissues. Many third-generation P-gp inhibitors such as elacridar, tariquidar, zosuquidar, etc...
April 3, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28367588/effect-of-long-term-in-vitro-lithium-exposure-on-mrna-levels-of-claudin-3-cyp1a1-abcg2-and-gstm3-genes-in-the-hcmec-d3-human-brain-endothelial-cell-line
#2
Ramzi Shawahna, Kayathiri Ganeshamoorthy, Luo Huilong, Jean-Michel Scherrmann, Pierre-Olivier Couraud, Xavier Declèves
BACKGROUND AND OBJECTIVES: Lithium chloride (LiCl) has been shown to improve the tightness of brain endothelial cell monolayers in vitro by inhibition of the GSK-3β enzyme, activation of the Wnt/beta-catenin pathway and regulation of tight junction (TJ) protein expression. However, the effect of LiCl on the drug transporters and drug-metabolizing enzymes has not been addressed so far. The hCMEC/D3 cell line is a validated in vitro BBB model expressing transporters and drug-metabolizing enzymes (phase 1 and 2)...
April 3, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28349335/population-pharmacokinetics-to-model-the-time-varying-clearance-of-the-pegylated-asparaginase-oncaspar-%C3%A2-in-children-with-acute-lymphoblastic-leukemia
#3
Gudrun Würthwein, Claudia Lanvers-Kaminsky, Georg Hempel, Silke Gastine, Anja Möricke, Martin Schrappe, Mats O Karlsson, Joachim Boos
BACKGROUND AND OBJECTIVES: The pharmacokinetics of the polyethylene glycol (PEG)-conjugated asparaginase Oncaspar(®) are characterized by an increase in elimination over time. The focus of our analysis is the better understanding of this time-dependency. METHODS: In paediatric acute lymphoblastic leukemia therapy (AIEOP-BFM ALL 2009), two administrations of Oncaspar(®) (2500 U/m(2) intravenously) in induction phase (14-day interval) and one single administration in reinduction were followed by weekly monitoring of asparaginase activity...
March 27, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28283988/nicotine-population-pharmacokinetics-in-healthy-adult-smokers-a-retrospective-analysis
#4
Mathilde Marchand, Patrick Brossard, Henri Merdjan, Nicola Lama, Rolf Weitkunat, Frank Lüdicke
BACKGROUND AND OBJECTIVE: Characterizing nicotine pharmacokinetics is challenging in the presence of background exposure. We performed a combined retrospective population pharmacokinetic analysis of 8 trials, including exposure to Tobacco Heating System and cigarettes (both inhaled), nicotine nasal spray and oral nicotine gum. METHOD: Data from 4 single product use trials were used to develop a population pharmacokinetic model with Phoenix(®) NLME™ and to derive exposure parameters...
March 10, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28283987/evaluating-the-feasibility-of-use-of-a-foreign-reference-product-for-generic-drug-applications-a-retrospective-pilot-study
#5
Yi-Lin Wang, Li-Feng Hsu
BACKGROUND AND OBJECTIVES: The adoption of a domestic reference product in bioequivalence (BE) studies for generic drug applications is required by some countries. The objective of this study is to assess the feasibility of this by investigating whether innovative products from different countries are bioequivalent. METHODS: Data were collected from all generic drug applications received by the Taiwan regulatory authority 2012-2016. If a submission package contained BE studies, that generic product was compared separately with different reference products, and the resulting data included in this analysis...
March 10, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28276004/hydroxylation-metabolisms-of-crassicauline-a-in-rats-under-toxic-dose
#6
Xue Fan, Shan-Shan Yin, Xue-Jing Li, Kui Yang, Liang Xu, Ke Lan
BACKGROUND AND OBJECTIVES: Crassicauline A, a C19 diterpenoid alkaloid in Aconitum herbs, is an analgesic drug clinically used in China. The in vivo metabolism of crassicauline A is poorly understood, while potential bioactivation is anticipated via hydroxylation metabolism. This work, therefore, aimed to investigate the in vivo hydroxylation metabolism of crassicauline A in rats. METHODS: Using a de novo developed and validated UPLC-MS/MS method, excretion studies in rats were carried out to investigate the recoveries of crassicauline A and its hydroxylated metabolites in urine and feces...
March 8, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28260174/effect-of-gevokizumab-on-interleukin-1%C3%AE-mediated-cytochrome-p450-3a4-and-drug-transporter-repression-in-cultured-human-hepatocytes
#7
Amélie Moreau, Marc Le Vée, Elodie Jouan, Claire Denizot, Yannick Parmentier, Olivier Fardel
BACKGROUND AND OBJECTIVES: Gevokizumab is a potent anti-interleukin (IL)-1β neutralizing monoclonal antibody (mAb), which may be used for treating inflammatory or autoimmune diseases. The present study was designed to characterize the potential effects of this mAb towards well-established IL-1β-mediated repression of hepatic drug detoxifying proteins, like cytochrome P450 (CYP) 3A4 and drug transporters. METHODS: Primary cultured human hepatocytes were exposed to various concentrations of IL-1β in the absence or presence of gevokizumab (5 µg/mL); mRNA expression and activity of CYP3A4 and transporters were next determined...
March 4, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28255865/antioxidative-and-protective-actions-of-apigenin-in-a-paracetamol-induced-hepatotoxicity-rat-model
#8
Aleksandar Rašković, Slobodan Gigov, Ivan Čapo, Milica Paut Kusturica, Boris Milijašević, Sunčica Kojić-Damjanov, Nikola Martić
BACKGROUND AND OBJECTIVES: Apigenin is known to have various pharmacological properties without causing significant toxicity; however, hepatoprotective effect of apigenin is not often reported. The aim of our study was to investigate if the alterations in lipid peroxidation and antioxidant status are in favor to prove the efficacy of apigenin against paracetamol-induced hepatotoxicity. METHODS: The effect of apigenin on paracetamol-induced hepatotoxicity in rats was examined by determining biochemical parameters, histological assessment and oxidative status in liver homogenates...
March 2, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28236116/clinical-pharmacokinetic-and-pharmacodynamic-profile-of-lenvatinib-an-orally-active-small-molecule-multitargeted-tyrosine-kinase-inhibitor
#9
Ziad Hussein, Hitoshi Mizuo, Seiichi Hayato, Masayuki Namiki, Robert Shumaker
Lenvatinib is a multikinase inhibitor that targets vascular endothelial growth factor (VEGF) receptors 1-3, fibroblast growth factor receptors 1-4, platelet-derived growth factor receptor-alpha, and RET and KIT proto-oncogenes. Lenvatinib is approved for the treatment of radioiodine-refractory differentiated thyroid cancer in the United States (US), European Union (EU), Canada, Japan, and Switzerland. It is also approved in combination with everolimus for the treatment of advanced renal cell carcinoma following ≥1 VEGF-targeted treatment in the US and EU...
February 24, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28229434/preclinical-pharmacokinetics-and-pharmacodynamics-of-pinometostat-epz-5676-a-first-in-class-small-molecule-s-adenosyl-methionine-competitive-inhibitor-of-dot1l
#10
Nigel J Waters
Acute leukemias bearing mixed lineage leukemia (MLL) rearrangements are aggressive diseases characterized by a poor overall prognosis despite multi-agent chemotherapy. Aberrant fusion proteins involving the MLL histone methyltransferase (HMT) lead to recruitment of DOT1L, to a multi-protein complex resulting in aberrant methylation of histone H3 lysine 79 at MLL target genes, and ultimately enhanced expression of critical genes for hematopoietic differentiation, including HOXA9 and MEIS1, and as such defines the established mechanism for leukemogenesis in MLL-rearrangement (MLL-r) leukemias...
February 22, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28194579/prediction-of-tissue-to-plasma-ratios-of-basic-compounds-in-mice
#11
Prashant B Nigade, Jayasagar Gundu, K Sreedhara Pai, Kumar V S Nemmani
BACKGROUND: Majority of reported studies so far developed correlation regression equations using the rat muscle-to-plasma drug concentration ratio (Kp-muscle) to predict tissue-to-plasma drug concentration ratios (Kp-tissues). Use of regression equations derived from rat Kp-muscle may not be ideal to predict the mice tissue-Kps as there are species differences. OBJECTIVES: (i) To develop the linear regression equations using mouse tissue-Kps; (ii) to assess the correlation between organ blood flow and/or organ weight with tissue-Kps and (iii) compare the observed tissue-Kps from mice with corresponding predicted tissue-Kps using Richter's rat-Kp specific equations...
February 13, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28185143/characterization-of-1-aminobenzotriazole-and-ketoconazole-as-novel-inhibitors-of-monoamine-oxidase-mao-an-in-vitro-investigation
#12
Abdul Naveed Shaik, Barbara W LeDuc, Ansar A Khan
BACKGROUND AND OBJECTIVES: 1-Aminobenzotriazole, a known time-dependent inhibitor of cytochrome P450 (CYP) enzymes, and ketoconazole, a strong inhibitor of the human CYP3A4 isozyme, are used as standard probe inhibitors to characterize the CYP and/or non-CYP-mediated metabolism of xenobiotics. In the present investigation, 1-Aminobenzotriazole and ketoconazole are characterized as potent monoamine oxidase (MAO) inhibitors in vitro using mouse, rat and human liver microsomes and S9 fractions...
February 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27220743/methylphenidate-for-treating-adhd-a-naturalistic-clinical-study-of-methylphenidate-blood-concentrations-in-children-and-adults-with-optimized-dosage
#13
Maria D Chermá, Martin Josefsson, Irene Rydberg, Per Woxler, Tomas Trygg, Olle Hollertz, Per A Gustafsson
BACKGROUND: Methylphenidate (MPH), along with behavioral and psychosocial interventions, is the first-line medication to treat attention-deficit hyperactivity disorder (ADHD) in Sweden. The dose of MPH for good symptom control differs between patients. However, studies of MPH concentration measurement in ADHD treatment are limited. OBJECTIVE: To describe blood and oral fluid (OF) concentrations of MPH after administration of medication in patients with well-adjusted MPH treatment for ADHD, and to identify the most suitable matrix for accurate MPH concentration during treatment...
April 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27209586/a-two-period-open-label-single-dose-crossover-study-in-healthy-volunteers-to-evaluate-the-drug-drug-interaction-between-cimetidine-and-inhaled-extrafine-chf-5993
#14
Fabrizia Mariotti, Giorgia Ciurlia, Luca Spaccapelo, Annamaria Muraro, Daniela Acerbi
BACKGROUND AND OBJECTIVES: CHF 5993 is an extrafine 'triple therapy' combination of the long-acting muscarinic antagonist glycopyrronium bromide (GB), the long-acting β2-agonist formoterol fumarate (FF), and the inhaled corticosteroid beclometasone dipropionate (BDP). It is in development for chronic obstructive pulmonary disease and asthma delivered via pressurised metered-dose inhaler. METHODS: This two-period, open-label, crossover study examined the drug-drug interaction of CHF 5993 and cimetidine...
April 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27180066/pharmacokinetics-and-bioavailability-of-the-gnrh-analogs-in-the-form-of-solution-and-zn-2-suspension-after-single-subcutaneous-injection-in-female-rats
#15
Aleksandra Suszka-Świtek, Florian Ryszka, Barbara Dolińska, Renata Dec, Alojzy Danch, Łukasz Filipczyk, Ryszard Wiaderkiewicz
BACKGROUND AND OBJECTIVES: Although many synthetic gonadoliberin analogs have been developed, only a few of them, including buserelin, were introduced into clinical practice. Dalarelin, which differs from buserelin by just one aminoacid in the position 6 (D-Ala), is not widely used so far. Gonadotropin-releasing hormone (GnRH) analogs are used to treat many different illnesses and are available in different forms like solution for injection, nasal spray, microspheres, etc. Unfortunately, none of the above drug formulations can release the hormones for 24 h...
April 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28101841/influence-of-sex-and-food-on-the-bioavailability-and-the-r-to-s-conversion-of-ketoprofen-stereoisomers-in-humans
#16
LETTER
Pietro Fagiolino, Nikoletta Fotaki, Marta Vázquez
No abstract text is available yet for this article.
February 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28101840/stereoselective-conversion-of-ketoprofen-in-men-versus-women-from-two-different-oral-dosage-formulations-observations-and-introspection-of-the-pharmacokinetic-data
#17
LETTER
Ranjeet Prasad Dash, Nuggehally R Srinivas
No abstract text is available yet for this article.
February 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27743266/erratum-to-population-pharmacokinetic-modeling-of-oxcarbazepine-active-metabolite-in-chinese-patients-with-epilepsy
#18
Yunli Yu, Quanying Zhang, Wenjun Xu, Chengzhe Lv, Gang Hao
No abstract text is available yet for this article.
February 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27538882/enhancing-oral-absorption-of-%C3%AE-lapachone-progress-till-date
#19
Marival Bermejo, Victor Mangas-Sanjuan, Isabel Gonzalez-Alvarez, Marta Gonzalez-Alvarez
β-Lapachone is a naphthoquinone with high and diverse biological activity. It is useful to treat several pathologies, in particular cancer due to its ability to induce selective apoptosis in tumoral cells. Despite its advantages, β-lapachone's clinical applications are limited by its low solubility in biological fluids and its low specific distribution pattern. In the last decade various formulation strategies have been designed and developed in order to overcome these limitations and to make feasible its wide therapeutic use...
February 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27438788/metabolomics-of-methylphenidate-and-ethylphenidate-implications-in-pharmacological-and-toxicological-effects
#20
Ricardo Jorge Dinis-Oliveira
Methylphenidate (MPH) is primarily indicated for attention-deficit hyperactivity disorder and narcolepsy therapy. A marked individual variability in the dose-response has been observed, and therefore dosage must be titrated for optimal therapeutic effect with minimal toxicity. This variability has been claimed to be predominantly pharmacokinetic. Moreover, due to its similar pharmacodynamics to amphetamine, MPH has been abused and fatalities have been reported. This review aims to discuss metabolomics of MPH, namely by presenting all major and minor metabolites...
February 2017: European Journal of Drug Metabolism and Pharmacokinetics
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